Synthesis, radiosynthesis, and in vitro evaluation of [131I]-5-iodo-N-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-yl)-ethyl]-2-methoxy-benzamide as a potential tumor imaging agent

Yu Ping Xu; Min Yang; Dong Hui Pan

doi:10.1016/j.apradiso.2008.12.010

Synthesis, radiosynthesis, and in vitro evaluation of [131I]-5-iodo-N-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-yl)-ethyl]-2-methoxy-benzamide as a potential tumor imaging agent

Appl Radiat Isot. 2009 Apr;67(4):594-7. doi: 10.1016/j.apradiso.2008.12.010. Epub 2008 Dec 24.

Authors

Yu Ping Xu¹, Min Yang, Dong Hui Pan

Affiliation

¹ The Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Ministry of Health, 20 Qianrong Road, Wuxi 214063, China.

PMID: 19181532
DOI: 10.1016/j.apradiso.2008.12.010

Abstract

This work reports the synthesis, radiolabeling and preliminary in vitro evaluation of [(131)I]-5-iodo-N-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-yl)-ethyl]-2-methoxy-benzamide. The tributylstannylprecursor was synthesized with a yield of 38%. Radiolabeling was performed using an electrophilic iododestannylation. Tracer yield was 94%, radiochemical purity was >95%. The tracer showed high uptake in MCF-7 breast cancer cell line and therefore will be evaluated further.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzamides / chemical synthesis*
Cell Line, Tumor
Humans
Iodine Radioisotopes*
Isoquinolines / chemical synthesis*
Magnetic Resonance Spectroscopy
Neoplasms / diagnostic imaging*
Radionuclide Imaging
Radiopharmaceuticals / chemical synthesis*
Spectrometry, Mass, Electrospray Ionization

Substances

5-iodo-N-(2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl)-2-methoxybenzamide
Benzamides
Iodine Radioisotopes
Isoquinolines
Radiopharmaceuticals